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. 2004 Jun 21;14(12):3313-7.
doi: 10.1016/j.bmcl.2004.03.063.

Thiol-based SAHA analogues as potent histone deacetylase inhibitors

Takayoshi Suzuki  1 , Akiyasu Kouketsu, Azusa Matsuura, Arihiro Kohara, Shin-Ichi Ninomiya, Kohfuku Kohda, Naoki Miyata
Affiliations

Thiol-based SAHA analogues as potent histone deacetylase inhibitors

Takayoshi Suzuki et al. Bioorg Med Chem Lett. .

Abstract

In order to find novel nonhydroxamate histone deacetylase (HDAC) inhibitors, a series of thiol-based compounds modeled after suberoylanilide hydroxamic acid (SAHA) was synthesized, and their inhibitory effect on HDACs was evaluated. Compound 6, in which the hydroxamic acid of SAHA was replaced by a thiol, was found to be as potent as SAHA, and optimization of this series led to the identification of HDAC inhibitors more potent than SAHA.

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